期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 63, 期 -, 页码 645-654出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.03.005
关键词
Pyrazole; Schiff's base; Pyrrole; Anti-inflammatory; Analgesic; COX inhibition
Some novel 1,3,4-trisubstituted pyrazoles were synthesized and screened for their anti-inflammatory and analgesic activities as well as their ulcerogenic liability. They showed anti-inflammatory and analgesic activities with better GIT tolerance than the standard drug phenylbutazone. In addition, IC50 values for 5e and 8e were recorded. Compound 5e was found to be the most active one as anti-inflammatory and analgesic agent. On the other hand, COX-1/COX-2 isozyme selectivity was also done which showed equal inhibition to both isoforms. (c) 2013 Elsevier Masson SAS. All rights reserved.
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